Cediranib (AZD2171) - Moligand™, 10mM in DMSO , Vascular endothelial growth factor receptor inhibitor, CAS No.288383-20-0, Vascular endothelial growth factor receptor inhibitor

CAS: 288383-20-0 Cat. No.: C408684 Summenformel: C₂₅H₂₇FN₄O₃ Molekulargewicht: 450.52 EG-Nummer: 670-946-2

QUALITÄT & REINHEIT Moligand™, 10mM in DMSO

Synonyms

NSC-732208 | 4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

Cediranib (AZD2171, NSC-732208) is a highly potentVEGFR(KDR)inhibitor withIC50of <1 nM, also inhibits Flt1/4 withIC50of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and F
In vitro

Cediranib inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. Cediranib has been shown to block Flt1-associated kinase with IC50 of 5 nM and VEGF-C and VEGF-D receptor Flt-4 with IC50 less than 3 nM. In addition, the IC50 values for inhibition of c-Kit and PDGFRβ tyrosine kinase are 2 nM and 5 nM respectively. Furthermore, no inhibition of enzyme activity is observed when 10 μM Cediranib is assayed with 100 μM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations of Cediranib are needed to prevent tumor cell proliferation in vitro.

In vivo

Cediranib even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF-induced angiogenesis. Cediranib causes hypertrophy in bone growth plate and prevents luteal development in ovary. These are physiological processes that are dependent upon angiogenesis. Cediranib shows broad spectrum activity in human tumor models at doses that are well tolerated. Besides, Cediranib causes regression of vascular tissues in human lung tumor xenografts.
Cell Data

cell lines：NHL, DLBCL, MCL, AML and ALL cell lines

Concentrations：10 μM

Incubation Time：72 hours

Powder Purity:≥97%

Spezifikationen

Synonyme

NSC-732208 | 4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α,

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Vascular endothelial growth factor receptor inhibitor

Produkteigenschaften

ALogP

4.9

Namen und Kennungen

Isomere SMILES

CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5

Molekulargewicht

450.52

Reaxy-Rn

11404252

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11404252&ln=

Zugehörige Ziele (menschlich)

CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (2 Activities)

Discover Target: CSF1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DDR1 Tchem Epithelial discoidin domain-containing receptor 1 (2 Activities)

Discover Target: DDR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (4 Activities)

Discover Target: RET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

STK10 Tchem Serine/threonine-protein kinase 10 (1 Activities)

Discover Target: STK10

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

STK35 Tchem Serine/threonine-protein kinase 35 (1 Activities)

Discover Target: STK35

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 (5 Activities)

Discover Target: FLT4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (1 Activities)

Discover Target: FLT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR1 Tclin Fibroblast growth factor receptor 1 (1 Activities)

Discover Target: FGFR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 (2 Activities)

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLK Tchem STE20-like serine/threonine-protein kinase (2 Activities)

Discover Target: SLK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha (3 Activities)

Discover Target: PDGFRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRB Tclin Platelet-derived growth factor receptor beta (5 Activities)

Discover Target: PDGFRB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT1 Tclin Vascular endothelial growth factor receptor 1 (5 Activities)

Discover Target: FLT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (8 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ACSL5 Tchem Long-chain-fatty-acid--CoA ligase 5 (1 Activities)

Discover Target: ACSL5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 (1 Activities)

Discover Target: ABL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit (6 Activities)

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro DMSO: 50 mg/mL (199.01 mM); Water: 25 mg/mL (99.5 mM); Ethanol: 1 mg/mL (3.98 mM)